UPLC-MS/MS法分析大鼠口服苗药了哥王的有效成分芹菜素后血浆中的药物代谢动力学  

Pharmacokinetics of Apigenin of Miao Medicine Wikstromia indica in Rats Plasma After Oral Administration was Analyzed by UPLC-MS/MS

作　　者：冯果[1] 郑传奇[1] 李玮[1] 何新[2] 吴增光[2] FENG Guo;ZHENG Chuan-qi;LI Wei;HE Xin;WU Zeng-guang(Guiyang University of Chinese Medicine,Guiyang Guizhou 550025,China;Tianjin University of Traditional Chinese Medicine,Tianjin 300193,China)

机构地区：[1]贵阳中医学院,贵州贵阳550025 [2]天津中医药大学中药学院,天津300193

出　　处：《时珍国医国药》2018年第12期2873-2876,共4页Lishizhen Medicine and Materia Medica Research

基　　金：国家自然科学基金(81760766);贵州省科技计划项目(黔科合基础[2017]1007);国家中医药管理局省级中药炮制技术传承基地建设项目(国中医科技[2015]136号);贵州省中医药管理项目(QZYY-2016-073);贵阳中医学院项目(贵中医科院内[2016]40号;博士启动基金(贵中医博士基金[2017]1号)

摘　　要：目的探讨苗药了哥王的黄酮类有效成分芹菜素口服给药后在大鼠血浆中的药物代谢动力学。方法取健康SD雄性大鼠,口服灌胃给药后,分别于不同时间点取血,处理血浆样品。制备高、中、低浓度双样本质控(QC)样品,取空白血浆,建立血浆中药物的标准曲线,以西瑞香素为内标物质,采用Agilent ZorB ax XDB-C18(3. 5μm,2. 1mm×50mm)色谱柱,流动相A:水(含0. 15%甲酸),流动相B:乙腈(含0. 15%甲酸),梯度洗脱,流速:0. 45 mL·min-1,进样量:10μL,电喷雾正离子化质谱法监测血浆中芹菜素的血药浓度。结果芹菜素的线性关系良好(r=0. 998 1),线性范围为1～2000μg·L-1;日间和日内精密度RSD均<10%;准确度的相对回收率98. 2%～102. 0%,RSD <10. 0%;药动学参数为:达峰时间Tmax为2. 0 h,达峰浓度Cmax为(124. 10±15. 35)μg·L-1,MRT(0-t)、MRT(0-∞)和T1/2的值分别为(5. 07±0. 69) h、(5. 55±1. 10) h、(4. 10±1. 64) h; AUC(0-t)、AUC(0-∞)值分别为(606. 97±126. 78)μg·(L·h)-1、(620. 06±138. 80)μg·(L·h)-1。结论该方法简便、准确、重复性好,专属性强,可用于芹菜素的药动学研究。Objective Objective to investigate the pharmacokinetics of apigenin of Miao medicine Wikstromia indica in rats after oral administration. Methods Healthy male SD rats after oral administration,blood samples were collected at different time points,and Plasma were treatmented. Concentration double sample quality control( QC) samples of high,medium and low were preparated. The establishment of the standard curve of drugs in the plasma,to terfenadine as internal standard substance. Chromatographic conditions: Agilent ZorB ax XDB-C18( 3. 5 μm,2. 1 mm × 50 mm) chromatographic column,mobile phase A: water( containing 0. 15% formic acid),mobile phase B: acetonitrile( containing 0. 15% formic acid),gradient elution,flow rate:0. 45 mL·min^-1,sample volume: 10 μL. Plasma concentrations of apigenin in rats plasma were detected by electrospray ionization mass spectrometry. Results Have a good linear relationship of apigenin( r = 0. 998 1),linear range of 1 ~ 2000 μg·L^-1.Day and day precision RSD were less than 10%. The relative recovery rate was 98. 2%~ 102. 0%,and the RSD was less than10%. The pharmacokinetic parameters were as follows: the peak time of Tmaxwas 2. 0 h,the peak concentration of Cmaxwas( 124. 10 ± 15. 35)μg·L^-1,MRT( 0-t),MRT( 0-∞)and T1/2 values were( 5. 07 ± 0. 69) h、( 5. 55 ± 1. 10) h、( 4. 10 ± 1. 64) h,and AUC( 0-t),AUC( 0-∞)values were( 606. 97 ± 126. 78)μg·( L·h)^-1、( 620. 06 ±138. 80)μg·( L·h)^-1,respectively. Conclusion The method was simple,accurate,reproducible and specific,and can be used for the pharmacokinetic study of apigenin.

关 键 词：了哥王 芹菜素 UPLC-MS/MS 药动学 

分 类 号：R285.5[医药卫生—中药学]